BR112021019054A2 - Formas sólidas de um composto do modificador alostérico da proteína do núcleo do vhb - Google Patents
Formas sólidas de um composto do modificador alostérico da proteína do núcleo do vhbInfo
- Publication number
- BR112021019054A2 BR112021019054A2 BR112021019054A BR112021019054A BR112021019054A2 BR 112021019054 A2 BR112021019054 A2 BR 112021019054A2 BR 112021019054 A BR112021019054 A BR 112021019054A BR 112021019054 A BR112021019054 A BR 112021019054A BR 112021019054 A2 BR112021019054 A2 BR 112021019054A2
- Authority
- BR
- Brazil
- Prior art keywords
- solid forms
- hbv
- core protein
- allosteric modifier
- hbv core
- Prior art date
Links
- 239000007787 solid Substances 0.000 title abstract 4
- 230000003281 allosteric effect Effects 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003607 modifier Substances 0.000 title abstract 3
- 101710132601 Capsid protein Proteins 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000015181 infectious disease Diseases 0.000 abstract 2
- YLJBFYZGSKMBEZ-MBSDFSHPSA-N C(C)OC(=O)C=1[C@@H](N=C(NC1CN1C[C@@H]2N(CC1)C(N(C2)CC(C(=O)O)(C)C)=O)C=2SC=CN2)C2=C(C(=CC=C2)F)C Chemical compound C(C)OC(=O)C=1[C@@H](N=C(NC1CN1C[C@@H]2N(CC1)C(N(C2)CC(C(=O)O)(C)C)=O)C=2SC=CN2)C2=C(C(=CC=C2)F)C YLJBFYZGSKMBEZ-MBSDFSHPSA-N 0.000 abstract 1
- 102000007999 Nuclear Proteins Human genes 0.000 abstract 1
- 108010089610 Nuclear Proteins Proteins 0.000 abstract 1
- 229940124765 capsid inhibitor Drugs 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- 230000003612 virological effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
formas sólidas de um composto do modificador alostérico da proteína do núcleo do vhb. a presente invenção refere-se a novas formas sólidas de composto (i), 3-[(8as)-7-[[(4s)-5-etoxicarbonil-4-(3-fluoro-2-metil-fenil)-2-tiazol-2-il-1,4-di-hidropirimidin-6-il] metil]-3-oxo-5,6,8,8a-tetra-hidro-1h-imidazo[1,5-a]pirazin-2-il]-2,2-dimetil-ácido propanoico e composições farmacêuticas compreendendo formas sólidas dos mesmos divulgado neste documento, que pode ser usado como um inibidor de capsídeo de vhb (ou modificador alostérico de proteína nuclear de vhb) ou para o tratamento ou profilaxia de uma doença viral em um paciente relacionada à infecção por vhb ou uma doença causada por infecção por vhb.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019079543 | 2019-03-25 | ||
| PCT/EP2020/057937 WO2020193459A1 (en) | 2019-03-25 | 2020-03-23 | Solid forms of a compound of hbv core protein allosteric modifier |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112021019054A2 true BR112021019054A2 (pt) | 2021-11-30 |
Family
ID=70005624
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021019054A BR112021019054A2 (pt) | 2019-03-25 | 2020-03-23 | Formas sólidas de um composto do modificador alostérico da proteína do núcleo do vhb |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11873302B2 (pt) |
| EP (1) | EP3947383A1 (pt) |
| JP (1) | JP2022525522A (pt) |
| KR (1) | KR20210136078A (pt) |
| CN (1) | CN113614088A (pt) |
| AU (1) | AU2020249331A1 (pt) |
| BR (1) | BR112021019054A2 (pt) |
| CA (1) | CA3130596A1 (pt) |
| IL (1) | IL286599A (pt) |
| MX (1) | MX2021011614A (pt) |
| TW (1) | TW202102503A (pt) |
| WO (1) | WO2020193459A1 (pt) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101933844B1 (ko) * | 2014-03-07 | 2018-12-28 | 에프. 호프만-라 로슈 아게 | B형 간염 바이러스 감염의 치료 및 예방을 위한 6-융합된 헤테로아릴다이하이드로피리미딘 |
Family Cites Families (33)
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| DE10012549A1 (de) | 2000-03-15 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10012823A1 (de) | 2000-03-16 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10012824A1 (de) | 2000-03-16 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10013126A1 (de) | 2000-03-17 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10125131A1 (de) | 2001-05-23 | 2002-12-05 | Bayer Ag | Verfahren zur Spaltung des Methyl 4-(2-chlor-4-fluorphenyl)-2-(3,5-difluor-2-pyridinyl)-6-methyl-1,4-dihydro-5-pyrmidincarboxylat-Racemats |
| CN1926241A (zh) | 2004-02-27 | 2007-03-07 | 帝斯曼知识产权资产管理有限公司 | 用酶来制备对映异构体富集的β－2－氨基酸的方法 |
| WO2006033995A2 (en) | 2004-09-16 | 2006-03-30 | Valeant Research And Development | Thiazolidin-4-ones having anti-hepatitis b activity |
| US20090305382A1 (en) | 2005-09-22 | 2009-12-10 | The Scripps Research Institute | Alkoxy indolinone based protein kinase inhibitors |
| GB0701366D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
| CN100453542C (zh) | 2007-04-30 | 2009-01-21 | 广东东阳光药业有限公司 | 2-杂环取代的二氢嘧啶消旋化合物的拆分方法 |
| WO2009067547A1 (en) | 2007-11-19 | 2009-05-28 | Takeda Pharmaceutical Company Limited | Polo-like kinase inhibitors |
| PL2098526T3 (pl) | 2008-02-22 | 2014-06-30 | Neurotune Ag | Bicykliczne związki zawierające azot aktywne w stanach przewlekłego bólu |
| RU2496514C2 (ru) | 2008-06-05 | 2013-10-27 | Займоджинетикс, Инк. | Применение пэгилированных интерферонов типа iii для лечения гепатита с |
| WO2010023480A1 (en) | 2008-08-29 | 2010-03-04 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Saturated bicyclic heterocyclic derivatives as smo antagonists |
| WO2010069147A1 (zh) | 2008-12-17 | 2010-06-24 | 张中能 | 二氢嘧啶类化合物、其组合物及其应用 |
| CN102372706A (zh) | 2010-08-09 | 2012-03-14 | 江苏恒瑞医药股份有限公司 | 酞嗪酮类衍生物、其制备方法及其在医药上的应用 |
| PL2888241T3 (pl) | 2012-08-24 | 2017-12-29 | Sunshine Lake Pharma Co., Ltd. | 2,4,5,6-Podstawione pochodne 3,6-dihydropirymidyny jako inhibitory polimerazy wirusa zapalenia wątroby typu B (HBV) do leczenia np. przewlekłego zapalenia wątroby |
| JP6113285B2 (ja) | 2012-09-10 | 2017-04-12 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂ型肝炎ウイルス感染症の治療及び予防用の６−アミノ酸ヘテロアリールジヒドロピリミジン |
| WO2014184328A1 (en) | 2013-05-17 | 2014-11-20 | F. Hoffmann-La Roche Ag | 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| CN104650069B (zh) | 2013-11-19 | 2019-04-19 | 广东东阳光药业有限公司 | 4-甲基二氢嘧啶类化合物及其在药物中的应用 |
| KR101933844B1 (ko) * | 2014-03-07 | 2018-12-28 | 에프. 호프만-라 로슈 아게 | B형 간염 바이러스 감염의 치료 및 예방을 위한 6-융합된 헤테로아릴다이하이드로피리미딘 |
| WO2016016196A1 (en) | 2014-07-31 | 2016-02-04 | F. Hoffmann-La Roche Ag | Novel chiral resolution of 4-aryl-2-thiazol-2-yl-1,4-dihydropyrimidine-5-carboxylic acid esters |
| AR103222A1 (es) | 2014-12-23 | 2017-04-26 | Hoffmann La Roche | Procedimiento para la preparación de análogos de 4-fenil-5-alcoxicarbonil-2-tiazol-2-il-1,4-dihidropirimidina |
| KR20170113658A (ko) | 2015-03-16 | 2017-10-12 | 에프. 호프만-라 로슈 아게 | Tlr7 작용제 및 hbv 캡시드 조립 억제제를 사용하는 병용 치료 |
| CN108135979A (zh) | 2015-11-03 | 2018-06-08 | 豪夫迈·罗氏有限公司 | Hbv衣壳组装抑制剂和干扰素的组合疗法 |
| WO2017108630A1 (en) * | 2015-12-21 | 2017-06-29 | F. Hoffmann-La Roche Ag | Combination therapy of an hbsag inhibitor and an hbv capsid assembly inhibitor |
| AR107633A1 (es) * | 2016-02-19 | 2018-05-16 | Hoffmann La Roche | Procedimiento para la preparación del ácido 4-fenil-5-alcoxicarbonil-2-tiazol-2-il-1,4-dihidropirimidin-6-il-[metil]-3-oxo-5,6,8,8a-tetrahidro-1h-imidazo[1,5a]pirazin-2-il-carboxílico |
| WO2018036941A1 (en) | 2016-08-24 | 2018-03-01 | F. Hoffmann-La Roche Ag | Combination therapy of an hbv capsid assembly inhibitor and a nucleos(t)ide analogue |
| MX2019002678A (es) | 2016-09-13 | 2019-05-20 | Hoffmann La Roche | Tratamiento combinado con un agonista de tlr7 y un inhibidor de montaje de capsida de hbv. |
| TW201907009A (zh) | 2017-05-31 | 2019-02-16 | 加拿大商艾爾布圖斯生技公司 | 用於治療b型肝炎之治療組成物及方法 |
| EP3700573A1 (en) | 2017-10-24 | 2020-09-02 | Gilead Sciences, Inc. | Methods of treating patients co-infected with a virus and tuberculosis |
| US20220315588A1 (en) | 2019-06-06 | 2022-10-06 | Hoffmann-La Roche Inc. | Alternative process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid |
| JP2022548652A (ja) | 2019-09-20 | 2022-11-21 | エフ．ホフマン－ラ ロシュ アーゲー | コアタンパク質アロステリックモジュレータを使用してｈｂｖ感染を処置する方法 |
-
2020
- 2020-03-23 JP JP2021556217A patent/JP2022525522A/ja active Pending
- 2020-03-23 CN CN202080023475.6A patent/CN113614088A/zh active Pending
- 2020-03-23 BR BR112021019054A patent/BR112021019054A2/pt unknown
- 2020-03-23 CA CA3130596A patent/CA3130596A1/en active Pending
- 2020-03-23 MX MX2021011614A patent/MX2021011614A/es unknown
- 2020-03-23 WO PCT/EP2020/057937 patent/WO2020193459A1/en unknown
- 2020-03-23 EP EP20710759.0A patent/EP3947383A1/en active Pending
- 2020-03-23 KR KR1020217032073A patent/KR20210136078A/ko not_active Application Discontinuation
- 2020-03-23 AU AU2020249331A patent/AU2020249331A1/en active Pending
- 2020-03-24 US US16/828,408 patent/US11873302B2/en active Active
- 2020-03-24 TW TW109109858A patent/TW202102503A/zh unknown
-
2021
- 2021-09-22 IL IL286599A patent/IL286599A/en unknown
-
2023
- 2023-12-14 US US18/539,773 patent/US20240116941A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA3130596A1 (en) | 2020-10-01 |
| MX2021011614A (es) | 2021-10-13 |
| JP2022525522A (ja) | 2022-05-17 |
| TW202102503A (zh) | 2021-01-16 |
| EP3947383A1 (en) | 2022-02-09 |
| IL286599A (en) | 2021-10-31 |
| WO2020193459A1 (en) | 2020-10-01 |
| US20240116941A1 (en) | 2024-04-11 |
| US20200308178A1 (en) | 2020-10-01 |
| CN113614088A (zh) | 2021-11-05 |
| AU2020249331A1 (en) | 2021-09-23 |
| US11873302B2 (en) | 2024-01-16 |
| KR20210136078A (ko) | 2021-11-16 |
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